2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Early 2 Factor (E2F)

Early 2 Factor (E2F)

The Early 2 Factors (E2Fs) are a family of eight winged-helix transcription factors that are key to regulating cell cycle progression from G1 to S phase among other functions. E2F1, E2F2, and E2F3a are expressed in early G1 through S phase and are believed to promote S phase initiation by activating genes involved in the G1 to S phase transition18. E2F3b, E2F4, E2F6, E2F5, E2F7, and E2F8 act as repressors and are expressed later in the cell cycle. E2Fs participate in myriad cell biological processes including: the cell cycle, DNA repair, apoptosis, development, differentiation, and metabolism.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16667
    HLM006474
    		Inhibitor 98.44%
    HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 μM in A375 cells.
    HLM006474
  • HY-149209
    LL-K8-22
    		Inhibitor 99.06%
    LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
    LL-K8-22
  • HY-153278
    Q901
    		Inhibitor 98.38%
    Q901 (CDK7-IN-21) is a selective and potent CDK7 inhibitor with an IC50 of 10 nM. Q901 disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 can be used for the research of cancer, such as colon cancer and lung cancer.
    Q901
  • HY-153278A
    Q901 TFA
    		Inhibitor
    Q901 (CDK7-IN-21) TFA is a selective and potent CDK7 inhibitor with an IC50 of 10 nM. Q901 TFA disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 TFA can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 TFA can be used for the research of cancer, such as colon cancer and lung cancer.
    Q901 TFA
  • HY-117857
    MRT00033659
    		Inhibitor 99.77%
    MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 μM for CK1δ) and CHK1 (IC50=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.
    MRT00033659
  • HY-164184
    Ly101-4B
    		Inhibitor
    Ly101-4B is an apoptosis inducer and multi-target inhibitor with antiproliferative, antitumor and cycytotoxic effects. Ly101-4B reduces HSF1 expression, inhibits microRNA-214 synthesis, downregulates HSP27, HSP70 and HSP90 expression, while suppressing E2F-dependent transcriptional activity and downregulating its target genes. Ly101-4B induces caspase 3/7-mediated apoptosis by reducing DNA synthesis, inhibiting the cell cycle and G1/S phase transition, without affecting RNA synthesis or inducing necrosis. Ly101-4B is selective for pancreatic ductal adenocarcinoma cells with different genotypes and varying degrees of E2F dependence. Ly101-4B can be used in research related to epithelial ovarian cancer and pancreatic ductal adenocarcinoma.
    Ly101-4B
  • HY-182241
    JR4-187
    		Inhibitor
    JR4-187 is an orally active, copper-dependent anticancer agent. JR4-187 downregulates genes involved in oxidative phosphorylation, MYC targets and E2F targets in cancer cells, while upregulates genes involved in the TNF-α signaling pathway, p53 pathway and KRAS signaling pathway, and downregulates CTR1 protein. JR4-187 induces ROS production, apoptosis, copper-dependent cytotoxicity, and exhibits selective cytotoxicity against KRAS-mutant cancer cells. JR4-187 is well tolerated in mouse models of pancreatic cancer. JR4-187 can be used in research related to cancers such as pancreatic ductal adenocarcinoma, colon cancer and rectal cancer.
    JR4-187
  • HY-177627
    Edifoligide
    		Inhibitor
    Edifoligide is a decoy oligonucleotide that binds to and inhibits E2F transcription factors and thus may prevent neointimal hyperplasia and vein graft failure
    Edifoligide
  • HY-177627A
    Edifoligide sodium
    		Inhibitor
    Edifoligide sodium is a decoy oligonucleotide that binds to and inhibits E2F transcription factors and thus may prevent neointimal hyperplasia and vein graft failure
    Edifoligide sodium
  • HY-159728
    PROTAC PRMT3 degrader 1
    PROTAC PRMT3 degrader 1 is a selective PRMT3 PROTAC degrader with a DC50 of 2.566 μM. PROTAC PRMT3 degrader 1 forms a ternary complex with MDM2 E3 ubiquitin ligase to induce proteasomal and neddylation-dependent degradation of PRMT3. PROTAC PRMT3 degrader 1 activates intrinsic apoptosis, endoplasmic reticulum stress signaling pathways. PROTAC PRMT3 degrader 1 downregulates E2F, MYC, oxidative phosphorylation pathways. PROTAC PRMT3 degrader 1 reduces cellular asymmetric dimethylarginine (ADMA) levels. PROTAC PRMT3 degrader 1 inhibits acute leukemia cell growth. PROTAC PRMT3 degrader 1 acts with glycolysis inhibitor 2-DG to reduce ATP production, induce intrinsic apoptosis, drive synergistic antiproliferative effects. PROTAC PRMT3 degrader 1 can be used for the research of acute leukemia.
    PROTAC PRMT3 degrader 1
  • HY-175397
    Dth
    		Degrader
    Dth (DFHBI-thalidomide) is an RNA aptamer-based PROTAC degrader. Dth can degrade a variety of endogenous proteins (such as mCherry, p50, p65 and E2F1) by replacing the 3′ module on the RNA scaffold with the RNA aptamer corresponding to the target protein. Dth upregulates IκB-α and Bax, and downregulates Bcl-2 and VEGF. Dth generates green fluorescence upon binding to the Broccoli RNA aptamer, enabling the tracing of RNA scaffolds. Dth can be used in cancer-related research.
    Dth
  • HY-123612
    JAS239
    		Inhibitor
    JAS239 is a blood-brain barrier-permeable ChoK inhibitor. JAS239 inhibits phosphocholine synthesis and reduces the expression level of E2F1 protein. JAS239 exhibits near-infrared fluorescence properties. JAS239 exerts anti-tumor activity against glioblastoma. JAS239 can be used in studies related to glioblastoma.
    JAS239
Cat. No. Product Name / Synonyms Application Reactivity